Sanofi

Xavier Bon

Philippe Vayron

Corinne Leroy

Julia Mateos-Caro

Frederic Bailly

Denis Largeau

Laure Jourdin

Jean-Louis Delepine

Christine Biencourt

The invention relates to a method for preparing 5-amino-benzoyl-benzofuran derivatives having the general formula in which Ris hydrogen or an alkyl or aryl group and Ris hydrogen, an alkyl, alkoxy or dialkylaminoalkoxy group. According to the invention, the compounds having formula I are prepared by hydrogenating a 5-nitro-benzofuran derivative having the general formula in which Rand Rhave the same meaning as above in the presence of palladized charcoal as a catalyst and in an ether or a mixture of ether as a solvent, thus forming the desired compounds.

Method for preparing 5-amino-benzoyl-benzofuran derivatives

The disclosure relates to a process for preparing 5-aminobenzoylbenzofuran derivatives of formula I: in which Rand Rare as defined in the disclosure; by reduction of a 5-nitrobenzofuran derivative of formula II: using a hydrogen transfer agent, in the presence of palladium-on-charcoal as catalyst and in an ether or an ether mixture as solvent.

Process for preparing aminobenzoylbenzofuran derivatives

The disclosure relates to a process for preparing benzofuran derivatives of general formula I: in which R, R, and Rare as defined in the disclosure; by coupling the hydroxylamine with a diketone of general formula III: in order to form an oxime that is then cyclized by heating in order to form the desired compound.

Process for preparing benzofuran derivatives substituted at position 5

This disclosure relates to a process for preparing 5-aminobenzofuran derivatives of general formula (I): in which Rand Rare as defined in the description,by treating a 5-N-alkylamidobenzofuran derivative of general formula (II): in which R, R, and Rare as defined in the description, with a strong acid, so as to form an acid addition salt of the compound of formula (I), which salt is itself treated, if necessary, with a basic agent so as to form this compound of formula (I) in free base form.

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Paris, France

Xavier Bon